MONO- AND POLYNUCLEAR COMPLEXES OF PT(II) WITH POLYPYRIDYL LIGANDS SYNTHESIS, SPECTROSCOPIC AND STRUCTURAL CHARACTERIZATION AND CYTOTOXIC ACTIVITY

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Abstract

An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl2)2(bpp)2(l-PtCl2)](H2O)2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl2(l-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl2(NH2dpt) [NH2dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric analysis demonstrated that these complexes, particularly [PtCl2(l-tptz)PtClNCPh]Cl, were effective death inducers in human colon rectal carcinoma HT29 cells and their cytotoxic activity was higher than that exerted by cisplatin. Morphological analysis of treated HT29 cells, performed by fluorescence microscopy after Hoechst 33258 staining, showed the appearance of the typical features of apoptosis. Moreover, our results suggested that mitochondria are involved in apoptosis induced by Pt(II) complexes in HT29 cells as demonstrated by dissipation of mitochondrial transmembrane potential.
Lingua originaleEnglish
pagine (da-a)1473-1482
Numero di pagine10
RivistaJournal of Inorganic Biochemistry
Volume101
Stato di pubblicazionePublished - 2007

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HT29 Cells
Apoptosis
Ligands
Pyrazines
Bisbenzimidazole
Mitochondria
Fluorescence microscopy
Bioactivity
Scaffolds
Cisplatin
Cells
Fluorescence Microscopy
Membrane Potentials
DNA
Cell Survival
Colon
Staining and Labeling
Carcinoma
1,2,4-triazole
2,4,6-tris(2-pyridyl)-1,3,5-triazine

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Inorganic Chemistry

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@article{d49f5f98a4184c6c826e5af22d40506f,
title = "MONO- AND POLYNUCLEAR COMPLEXES OF PT(II) WITH POLYPYRIDYL LIGANDS SYNTHESIS, SPECTROSCOPIC AND STRUCTURAL CHARACTERIZATION AND CYTOTOXIC ACTIVITY",
abstract = "An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl2)2(bpp)2(l-PtCl2)](H2O)2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl2(l-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl2(NH2dpt) [NH2dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric analysis demonstrated that these complexes, particularly [PtCl2(l-tptz)PtClNCPh]Cl, were effective death inducers in human colon rectal carcinoma HT29 cells and their cytotoxic activity was higher than that exerted by cisplatin. Morphological analysis of treated HT29 cells, performed by fluorescence microscopy after Hoechst 33258 staining, showed the appearance of the typical features of apoptosis. Moreover, our results suggested that mitochondria are involved in apoptosis induced by Pt(II) complexes in HT29 cells as demonstrated by dissipation of mitochondrial transmembrane potential.",
author = "Giuseppe Calvaruso and Santino Orecchio and Gianfranco Fontana and Simona Rubino and Patrizia Portanova and Antonella Albanese",
year = "2007",
language = "English",
volume = "101",
pages = "1473--1482",
journal = "Journal of Inorganic Biochemistry",
issn = "0162-0134",
publisher = "Elsevier Inc.",

}

TY - JOUR

T1 - MONO- AND POLYNUCLEAR COMPLEXES OF PT(II) WITH POLYPYRIDYL LIGANDS SYNTHESIS, SPECTROSCOPIC AND STRUCTURAL CHARACTERIZATION AND CYTOTOXIC ACTIVITY

AU - Calvaruso, Giuseppe

AU - Orecchio, Santino

AU - Fontana, Gianfranco

AU - Rubino, Simona

AU - Portanova, Patrizia

AU - Albanese, Antonella

PY - 2007

Y1 - 2007

N2 - An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl2)2(bpp)2(l-PtCl2)](H2O)2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl2(l-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl2(NH2dpt) [NH2dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric analysis demonstrated that these complexes, particularly [PtCl2(l-tptz)PtClNCPh]Cl, were effective death inducers in human colon rectal carcinoma HT29 cells and their cytotoxic activity was higher than that exerted by cisplatin. Morphological analysis of treated HT29 cells, performed by fluorescence microscopy after Hoechst 33258 staining, showed the appearance of the typical features of apoptosis. Moreover, our results suggested that mitochondria are involved in apoptosis induced by Pt(II) complexes in HT29 cells as demonstrated by dissipation of mitochondrial transmembrane potential.

AB - An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl2)2(bpp)2(l-PtCl2)](H2O)2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl2(l-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl2(NH2dpt) [NH2dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric analysis demonstrated that these complexes, particularly [PtCl2(l-tptz)PtClNCPh]Cl, were effective death inducers in human colon rectal carcinoma HT29 cells and their cytotoxic activity was higher than that exerted by cisplatin. Morphological analysis of treated HT29 cells, performed by fluorescence microscopy after Hoechst 33258 staining, showed the appearance of the typical features of apoptosis. Moreover, our results suggested that mitochondria are involved in apoptosis induced by Pt(II) complexes in HT29 cells as demonstrated by dissipation of mitochondrial transmembrane potential.

UR - http://hdl.handle.net/10447/19004

M3 - Article

VL - 101

SP - 1473

EP - 1482

JO - Journal of Inorganic Biochemistry

JF - Journal of Inorganic Biochemistry

SN - 0162-0134

ER -